Details
Stereochemistry | ACHIRAL |
Molecular Formula | C25H34FN3O2 |
Molecular Weight | 427.5548 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)COC1=CC=C(CNC(=O)N(CC2=CC=C(F)C=C2)C3CCN(C)CC3)C=C1
InChI
InChIKey=RKEWSXXUOLRFBX-UHFFFAOYSA-N
InChI=1S/C25H34FN3O2/c1-19(2)18-31-24-10-6-20(7-11-24)16-27-25(30)29(23-12-14-28(3)15-13-23)17-21-4-8-22(26)9-5-21/h4-11,19,23H,12-18H2,1-3H3,(H,27,30)
DescriptionCurator's Comment: Description was created based on several sources, including
http://www.acadia-pharm.com/product/
Curator's Comment: Description was created based on several sources, including
http://www.acadia-pharm.com/product/
Pimavanserin, marketed under the trade name Nuplazid, a non-dopaminergic atypical antipsychotic developed by Acadia Pharmaceuticals is the first and only medication approved by the U.S. Food and Drug Administration (FDA) for the treatment of hallucinations and delusions associated with Parkinson’s disease psychosis. The mechanism of action of pimavanserin in the treatment of hallucinations and delusions associated with Parkinson’s disease psychosis is unknown. However, the effect of pimavanserin could be mediated through a combination of inverse agonist and antagonist activity at serotonin 5-HT2A receptors and to a lesser extent at serotonin 5-HT2C receptors. In vitro, pimavanserin acts as an inverse agonist and antagonist at serotonin 5-HT2A receptors with high binding affinity (Ki value 0.087 nM) and at serotonin 5-HT2C receptors with lower binding affinity (Ki value 0.44 nM). Pimavanserin shows low binding to sigma 1 receptors (Ki value 120 nM) and has no appreciable affinity (Ki value >300 nM), to serotonin 5-HT2B, dopaminergic (including D2), muscarinic, histaminergic, or adrenergic receptors, or to calcium channels. Pimavanserin was approved by the FDA to treat hallucinations and delusions associated with psychosis experienced by some people with Parkinson's disease on April 29, 2016.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24682754
Curator's Comment: Pimavanserin readily crosses the blood brain barrier and acts as a CNS-active 5-HT2A inverse agonist.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
0.087 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Nuplazid Approved UseNUPLAZID is indicated for the treatment of hallucinations and delusions associated with Parkinson’s disease
psychosis Launch Date2016 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
151.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
300 mg single, nasogastric dose: 300 mg route of administration: Nasogastric experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
20.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
92.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
49.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
100 mg single, nasogastric dose: 100 mg route of administration: Nasogastric experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
193.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
247.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
9.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
111.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
200 mg single, nasogastric dose: 200 mg route of administration: Nasogastric experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
10798 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
300 mg single, nasogastric dose: 300 mg route of administration: Nasogastric experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1315 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1838.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3742 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
100 mg single, nasogastric dose: 100 mg route of administration: Nasogastric experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3804.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4680.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
706 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
7335 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
200 mg single, nasogastric dose: 200 mg route of administration: Nasogastric experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
53.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
300 mg single, nasogastric dose: 300 mg route of administration: Nasogastric experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
53 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
54.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
58.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
100 mg single, nasogastric dose: 100 mg route of administration: Nasogastric experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
60.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
48 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
57 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
55.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
200 mg single, nasogastric dose: 200 mg route of administration: Nasogastric experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.2% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17473118 |
300 mg single, nasogastric dose: 300 mg route of administration: Nasogastric experiment type: SINGLE co-administered: |
PIMAVANSERIN TARTRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
150 mg 1 times / day multiple, oral Highest studied dose Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: |
healthy, 23.8 years (range: 19-28 years) n = 6 Health Status: healthy Age Group: 23.8 years (range: 19-28 years) Sex: M Population Size: 6 Sources: |
Disc. AE: Nausea, Vomiting... Other AEs: Gastrointestinal disorders, Nervous system disorders... AEs leading to discontinuation/dose reduction: Nausea (1 patient) Other AEs:Vomiting (2 patients) Dyspepsia (1 patient) Gastrointestinal disorders (5 patients) Sources: Nervous system disorders (6 patients) General system disorders NEC (3 patients) |
100 mg 1 times / day multiple, oral Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
healthy, 23.8 years (range: 19-28 years) n = 6 Health Status: healthy Age Group: 23.8 years (range: 19-28 years) Sex: M Population Size: 6 Sources: |
Disc. AE: Nausea, Vomiting... AEs leading to discontinuation/dose reduction: Nausea (1 patient) Sources: Vomiting (1 patient) |
300 mg single, nasogastric Highest studied dose Dose: 300 mg Route: nasogastric Route: single Dose: 300 mg Sources: |
healthy, 25.8 years (range: 25-28 years) n = 4 Health Status: healthy Age Group: 25.8 years (range: 25-28 years) Sex: M Population Size: 4 Sources: |
Other AEs: Nervous system disorders, General system disorders NEC... Other AEs: Nervous system disorders (2 patients) Sources: General system disorders NEC (1 patient) Vascular disorders (1 patient) |
50 mg single, oral Highest studied dose |
healthy, 25.8 years (range: 25-28 years) n = 4 Health Status: healthy Age Group: 25.8 years (range: 25-28 years) Sex: M Population Size: 4 Sources: |
Other AEs: Cardiac disorders, Gastrointestinal disorders... Other AEs: Cardiac disorders (1 patient) Sources: Gastrointestinal disorders (2 patients) Nervous system disorders (2 patients) |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: Page: 109 |
unhealthy, 71 years (range: 41-85 years) n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: 71 years (range: 41-85 years) Sex: M+F Population Size: 202 Sources: Page: 109 |
Disc. AE: Confusional state, Psychotic disorder... AEs leading to discontinuation/dose reduction: Confusional state (0.5%) Sources: Page: 109Psychotic disorder (1.5%) Mental status changes (1.5%) Headache (0.5%) Asthenia (0.5%) Infections and infestations (1%) Urinary tract infection (1%) Pollakiuria (0.5%) Dehydration (0.5%) Respiratory distress (0.5%) |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: |
unhealthy, > 40 years n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: > 40 years Sex: M+F Population Size: 202 Sources: |
Disc. AE: Hallucination, Fatigue... AEs leading to discontinuation/dose reduction: Hallucination (2%) Sources: Fatigue (1%) |
17 mg 2 times / day multiple, oral Recommended Dose: 17 mg, 2 times / day Route: oral Route: multiple Dose: 17 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Condition: dementia-related psychosis Sources: |
Other AEs: Heart failure, Pneumonia... Other AEs: Heart failure (grade 5) Sources: Pneumonia (grade 5) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Dyspepsia | 1 patient Disc. AE |
150 mg 1 times / day multiple, oral Highest studied dose Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: |
healthy, 23.8 years (range: 19-28 years) n = 6 Health Status: healthy Age Group: 23.8 years (range: 19-28 years) Sex: M Population Size: 6 Sources: |
Nausea | 1 patient Disc. AE |
150 mg 1 times / day multiple, oral Highest studied dose Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: |
healthy, 23.8 years (range: 19-28 years) n = 6 Health Status: healthy Age Group: 23.8 years (range: 19-28 years) Sex: M Population Size: 6 Sources: |
Vomiting | 2 patients Disc. AE |
150 mg 1 times / day multiple, oral Highest studied dose Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: |
healthy, 23.8 years (range: 19-28 years) n = 6 Health Status: healthy Age Group: 23.8 years (range: 19-28 years) Sex: M Population Size: 6 Sources: |
General system disorders NEC | 3 patients | 150 mg 1 times / day multiple, oral Highest studied dose Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: |
healthy, 23.8 years (range: 19-28 years) n = 6 Health Status: healthy Age Group: 23.8 years (range: 19-28 years) Sex: M Population Size: 6 Sources: |
Gastrointestinal disorders | 5 patients | 150 mg 1 times / day multiple, oral Highest studied dose Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: |
healthy, 23.8 years (range: 19-28 years) n = 6 Health Status: healthy Age Group: 23.8 years (range: 19-28 years) Sex: M Population Size: 6 Sources: |
Nervous system disorders | 6 patients | 150 mg 1 times / day multiple, oral Highest studied dose Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: |
healthy, 23.8 years (range: 19-28 years) n = 6 Health Status: healthy Age Group: 23.8 years (range: 19-28 years) Sex: M Population Size: 6 Sources: |
Nausea | 1 patient Disc. AE |
100 mg 1 times / day multiple, oral Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
healthy, 23.8 years (range: 19-28 years) n = 6 Health Status: healthy Age Group: 23.8 years (range: 19-28 years) Sex: M Population Size: 6 Sources: |
Vomiting | 1 patient Disc. AE |
100 mg 1 times / day multiple, oral Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
healthy, 23.8 years (range: 19-28 years) n = 6 Health Status: healthy Age Group: 23.8 years (range: 19-28 years) Sex: M Population Size: 6 Sources: |
General system disorders NEC | 1 patient | 300 mg single, nasogastric Highest studied dose Dose: 300 mg Route: nasogastric Route: single Dose: 300 mg Sources: |
healthy, 25.8 years (range: 25-28 years) n = 4 Health Status: healthy Age Group: 25.8 years (range: 25-28 years) Sex: M Population Size: 4 Sources: |
Vascular disorders | 1 patient | 300 mg single, nasogastric Highest studied dose Dose: 300 mg Route: nasogastric Route: single Dose: 300 mg Sources: |
healthy, 25.8 years (range: 25-28 years) n = 4 Health Status: healthy Age Group: 25.8 years (range: 25-28 years) Sex: M Population Size: 4 Sources: |
Nervous system disorders | 2 patients | 300 mg single, nasogastric Highest studied dose Dose: 300 mg Route: nasogastric Route: single Dose: 300 mg Sources: |
healthy, 25.8 years (range: 25-28 years) n = 4 Health Status: healthy Age Group: 25.8 years (range: 25-28 years) Sex: M Population Size: 4 Sources: |
Cardiac disorders | 1 patient | 50 mg single, oral Highest studied dose |
healthy, 25.8 years (range: 25-28 years) n = 4 Health Status: healthy Age Group: 25.8 years (range: 25-28 years) Sex: M Population Size: 4 Sources: |
Gastrointestinal disorders | 2 patients | 50 mg single, oral Highest studied dose |
healthy, 25.8 years (range: 25-28 years) n = 4 Health Status: healthy Age Group: 25.8 years (range: 25-28 years) Sex: M Population Size: 4 Sources: |
Nervous system disorders | 2 patients | 50 mg single, oral Highest studied dose |
healthy, 25.8 years (range: 25-28 years) n = 4 Health Status: healthy Age Group: 25.8 years (range: 25-28 years) Sex: M Population Size: 4 Sources: |
Asthenia | 0.5% Disc. AE |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: Page: 109 |
unhealthy, 71 years (range: 41-85 years) n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: 71 years (range: 41-85 years) Sex: M+F Population Size: 202 Sources: Page: 109 |
Confusional state | 0.5% Disc. AE |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: Page: 109 |
unhealthy, 71 years (range: 41-85 years) n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: 71 years (range: 41-85 years) Sex: M+F Population Size: 202 Sources: Page: 109 |
Dehydration | 0.5% Disc. AE |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: Page: 109 |
unhealthy, 71 years (range: 41-85 years) n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: 71 years (range: 41-85 years) Sex: M+F Population Size: 202 Sources: Page: 109 |
Headache | 0.5% Disc. AE |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: Page: 109 |
unhealthy, 71 years (range: 41-85 years) n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: 71 years (range: 41-85 years) Sex: M+F Population Size: 202 Sources: Page: 109 |
Pollakiuria | 0.5% Disc. AE |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: Page: 109 |
unhealthy, 71 years (range: 41-85 years) n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: 71 years (range: 41-85 years) Sex: M+F Population Size: 202 Sources: Page: 109 |
Respiratory distress | 0.5% Disc. AE |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: Page: 109 |
unhealthy, 71 years (range: 41-85 years) n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: 71 years (range: 41-85 years) Sex: M+F Population Size: 202 Sources: Page: 109 |
Infections and infestations | 1% Disc. AE |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: Page: 109 |
unhealthy, 71 years (range: 41-85 years) n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: 71 years (range: 41-85 years) Sex: M+F Population Size: 202 Sources: Page: 109 |
Urinary tract infection | 1% Disc. AE |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: Page: 109 |
unhealthy, 71 years (range: 41-85 years) n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: 71 years (range: 41-85 years) Sex: M+F Population Size: 202 Sources: Page: 109 |
Mental status changes | 1.5% Disc. AE |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: Page: 109 |
unhealthy, 71 years (range: 41-85 years) n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: 71 years (range: 41-85 years) Sex: M+F Population Size: 202 Sources: Page: 109 |
Psychotic disorder | 1.5% Disc. AE |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: Page: 109 |
unhealthy, 71 years (range: 41-85 years) n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: 71 years (range: 41-85 years) Sex: M+F Population Size: 202 Sources: Page: 109 |
Fatigue | 1% Disc. AE |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: |
unhealthy, > 40 years n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: > 40 years Sex: M+F Population Size: 202 Sources: |
Hallucination | 2% Disc. AE |
34 mg 1 times / day multiple, oral Recommended Dose: 34 mg, 1 times / day Route: oral Route: multiple Dose: 34 mg, 1 times / day Sources: |
unhealthy, > 40 years n = 202 Health Status: unhealthy Condition: hallucinations and delusions associated with Parkinson’s disease psychosis Age Group: > 40 years Sex: M+F Population Size: 202 Sources: |
Heart failure | grade 5 | 17 mg 2 times / day multiple, oral Recommended Dose: 17 mg, 2 times / day Route: oral Route: multiple Dose: 17 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Condition: dementia-related psychosis Sources: |
Pneumonia | grade 5 | 17 mg 2 times / day multiple, oral Recommended Dose: 17 mg, 2 times / day Route: oral Route: multiple Dose: 17 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Condition: dementia-related psychosis Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes | yes (co-administration study) Comment: Ketoconazole increased Pimavanserin Cmax and AUC by 1.5- and 3- fold, respectively Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/207318Orig1s000ClinPharmR.pdf#page=9 Page: 9.0 |
|||
yes | yes (co-administration study) Comment: Ketoconazole increased Pimavanserin Cmax and AUC by 1.5- and 3- fold, respectively Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/207318Orig1s000ClinPharmR.pdf#page=2 Page: 2.0 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/207318Orig1s000ClinPharmR.pdf#page=51 Page: 51.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist. | 2006 May |
|
5-HT(2A) inverse-agonists for the treatment of insomnia. | 2008 |
|
Pimavanserin tartrate: a 5-HT2A inverse agonist with potential for treating various neuropsychiatric disorders. | 2008 Dec |
|
Aripiprazole's receptor pharmacology and extrapyramidal side effects. | 2008 Mar |
|
PET analysis of the 5-HT2A receptor inverse agonist ACP-103 in human brain. | 2008 Mar |
|
A 5-HT2A receptor inverse agonist, ACP-103, reduces tremor in a rat model and levodopa-induced dyskinesias in a monkey model. | 2008 Oct |
|
Attenuation of phencyclidine-induced object recognition deficits by the combination of atypical antipsychotic drugs and pimavanserin (ACP 103), a 5-hydroxytryptamine(2A) receptor inverse agonist. | 2010 Feb |
|
Parkinson's disease dementia. | 2010 Jul |
|
Serotonin 5-HT(2A) receptor antagonists in the treatment of insomnia: present status and future prospects. | 2010 Mar |
|
Pimavanserin, a serotonin(2A) receptor inverse agonist, for the treatment of parkinson's disease psychosis. | 2010 Mar |
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Pimavanserin for the treatment of Parkinson's disease psychosis. | 2013 Oct |
Patents
Sample Use Guides
The recommended dose of NUPLAZID (Pimavanserin) is 34 mg, taken orally as two 17 mg strength tablets once daily, without
titration. Pimavanserin can be taken with or without food.
Route of Administration:
Oral
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